Patch

Abstract

A Bisoprolol patch, wherein the skin penetration rate of Bisoprolol after 24 hours is 15 to 60% of the maximum skin penetration rate thereof, shows a little difference between the maximum level of the concentration in blood and the minimum level thereof in repeated administration and, therefore, scarcely exhibits side effects. Moreover, it achieves the quick development of the drug effect owing to the stabilization of the concentration in blood within a short time.

Description

[0001]This patent application is a divisional of U.S. application Ser. No. 11 / 814,840, filed Jul. 26, 2007, which is the U.S. National Stage of International Application No. PCT / JP2006 / 300419 filed Jan. 16, 2006, which claims the benefit of priority from Japanese Application No. 2005-024049 filed Jan. 31, 2005, each of which are herein incorporated by reference in their entirety.TECHNICAL FIELD[0002]The invention relates to a patch comprising Bisoprolol which is a β-blocker.BACKGROUND ART[0003]As administration methods for drugs, an oral administration using tablets, capsules, syrups and the like has been made in many drugs. However, in case of the oral administration, there were drawbacks that it lacked in duration of the effect, an unnecessary high blood concentration was recognized for a while after the administration, whereby a side effect occurred easily, and the like.[0004]Bisoprolol is high in β1-receptor selectivity and a β-blocker which does not have an intrinsic sympathomi...

AI Technical Summary

Benefits of technology

[0024]By a Bisoprolol patch of the invention, it is possible to provide a safe patch, wherein it shows a little difference between the maximum level of the concentration in blood and the minimum level thereof even in repeated administration necessary for therapy of the essential hypertension, and therefore, scarcely exhibits serious side effects due to an excess hypotension, and moreover, achieves the quick development of the drug effect owing to the stabilization of the concentration in blood within a short time, and moreover, skin irritation is scarce.BEST EMBODIMENT FOR CARRYING OUT THE INVENTION

[0025]In the following, the patch of the invention is illustrated in more detail.

[0026]The patch of the invention indicates a patch containing at least a backing and a pressure-sensitive adhesive layer composition and comprises an external patch of reservoir type and an external patch of matrix type which are called generally. Comparing the external patch of reservoir type and the external patch of matrix type, generally, the external patch of matrix type, in which a composition of a pressure-sensitive adhesive layer having a self adhesive force adheres directly to the skin, is more excellent in adhesiveness and is also excellent in penetration of a drug to the skin, and therefore, in the following the patch of the invention is mainly explained taking a patch of matrix type as an example, though it is not limited this.

[0027]In addition, a hydrophobic polymer in the specification is a polymer using an organic solvent or an organic solvent mixture as solvents for polymer when preparing a pressure-sensitive adhesive layer of the patch.

[0028]The patch of the invention is typically a form which consists of a hydrophobic matrix (pressure-sensitive adhesive layer) containing a drug (Bisoprolol and / or a pharmaceutically acceptable salt thereof) as is shown in FIG. 6, and a backing on its back. Although it is preferable that this pressure-sensitive adhesive layer has an adhesive force to maintain an effective area on a surface of the skin without problem for therapy for at least 12 or more hours, in a case that it is difficult, it is possible to use a sheet type cover which has a larger area compared with a layer containing the drug and also has an adhesive force.

[0029]Bisoprolol which can be used in the invention may be a free form or its salt. In case of using the salt, it is not particularly limited if it is a pharmaceutically acceptable salt, however, preferably fumarate, hydrochloride, sulfonate, mesylate, citrate, tartarate, maleate or acetate. Among these, Bisoprolol hemifumarate is more preferable.

Problems solved by technology

However, in case of the oral administration, there were drawbacks that it lacked in duration of the effect, an unnecessary high blood concentration was recognized for a while after the administration, whereby a side effect occurred easily, and the like.

Although Bisoprolol is relatively little in the effect to bronchus due to the high β1 selectivity, there are cases that symptoms such as bradycardia, dizziness and physical weariness occur, and there were problems in the point of stabilization of the concentration in blood and sustainability of the effect.

However, although this patch attained almost constant and stable skin penetration rate (FIG. 1 and FIG. 2 in patent document 1), there were inconveniences such as difficulty to obtain an effective blood concentration for therapy or necessity to take much time till the blood concentration when repeating administration was stabilized.

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